Ligands organométalliques

<p>Dual inhibitor of the adaptor protein 2-associated kinase 1 (AAK1) and BMP2-inducible kinase (BMP2K) with IC50 values of 270 nM and 1 μM, respectively. In a recent study, SGC AAK1 1 stabilised β-catenin, inhibited phosphorylation of the AP2 complex subunit mu protein (AP2M1) and activated Wnt signalling in in vitro experiments._x000D_</p>

<p>Rigosertib sodium is an experimental chemotherapeutic agent that is a derivative of benzyl styryl sulfone. It is synthesized chemically and functions primarily by inhibiting key signaling pathways involved in cancer cell proliferation. Specifically, Rigosertib targets the RAS signaling pathway along with the phosphatidylinositol-3-kinase/AKT and polo-like kinase 1 (Plk1) pathways, impeding the progression of the cell cycle and inducing apoptosis in malignant cells.</p>

<p>Tretinoin is a type of retinoic acid that can be used for the treatment of acne. It is a chemical inhibitor that binds to nuclear receptors and leads to an increase in apoptosis. This type of retinoic acid helps with cell detachment and increases shedding thus increasing cell turnover. Tretinoin has been shown to have antibacterial efficacy against Staphylococcus aureus, as well as synergistic effects when combined with other agents, such as cyclic lipopeptide antibiotics and quinolones. Additionally, Tretinoin is used in the research and treatment for promyelocytic leukaemia.</p>

<p>Inhibits interaction between small GTPase Rab27a and its effector JFC1 (synaptotagmin-like protein1, Slp1). These proteins regulate neutrophil exocytosis, decrease neutrophil infiltration in liver and kidneys and reduce extracellular ROS production by NAPDH oxidase. Thus, nexinhibib20 suppresses systemic inflammation.</p>

<p>Selective inhibitor of the platelet derived growth factor receptor PDGFRβ with IC50 value of 4.2 nM. JNJ 10198409 inhibits the PDGFRβ kinase activity and its downstream signalling leading to anti-proliferative and anti-angiogenic effects, which were confirmed in various tumoral cell lines.</p>

<p>Vildagliptin is an antihyperglycemic agent that is used for the management of type 2 diabetes mellitus. This drug is a dipeptidyl peptidase 4 inhibitor and prevents the degradation of glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This leads to improved glycemic control.</p>

<p>mGluR5 antagonist</p>

<p>A calcium-binding protein S100A9 inhibitor with immunomodulatory activity that reduces pathology in experimental collagenase-induced osteoarthritis.</p>

<p>Inhibitor of ERK1 and ERK2 serine/threonine kinases</p>

<p>Fluvastatin is a statin that lowers blood cholesterol and triglycerides by inhibiting HMG-CoA reductase, an enzyme that plays a critical role in the synthesis of cholesterol. Fluvastatin has also been shown to reduce the incidence of myocardial infarction, and to reduce atherosclerotic lesions in animal models, reducing the incidence of cardiovascular disease. Fluvastatin also has been shown to inhibit the activation of toll-like receptor 4 (TLR4) by lipopolysaccharide (LPS), which may be related to its anti-inflammatory effects. Furthermore, through lowering blood cholesterol, Fluvastatin also inhibits tubulointerstitial injury and prevents renal damage caused by high concentrations of the lipid.</p>

<p>MK 886 is a leukotriene antagonist that has been studied for use in treating atherosclerosis. This drug inhibits the 5-lipoxygenase activating protein thus inhibiting 5-lipoxygenase.</p>

<p>Brimonidine-D-tartrate is a selective alpha-2 adrenergic agonist, which is a pharmacological compound derived synthetically, targeting specific receptor subtypes in the adrenergic receptor family. Its mode of action involves reducing aqueous humor production and increasing uveoscleral outflow in the eye, thereby lowering intraocular pressure. Additionally, it induces peripheral vasoconstriction, playing a role in reducing redness in rosacea.</p>

<p>Synthetic estradiol derivative</p>

<p>Dapoxetine is a drug that belongs to the group of selective serotonin reuptake inhibitors (SSRIs). It is used to treat premature ejaculation. This drug inhibits the serotonin transporter allowing for an increased action of serotonin at the postsynaptic cleft, thus promoting ejaculatory delay.</p>

<p>Vipivotide tetraxetan is a radioactive therapeutic agent, which is a radioligand conjugate composed of a DOTA chelator linked to a targeting moiety. The source of this compound lies in its synthesis, where the DOTA ligand is conjugated to a peptide or small molecule that targets specific cell surface antigens expressed on cancer cells.</p>

<p>Sulindac is a non-steroidal anti-inflammatory drug that has anti-inflammatory and analgesic properties. It is used to relieve the pain of osteoarthritis and rheumatoid arthritis by reducing inflammation and inhibiting the production of prostaglandins, which are chemicals that cause inflammation.</p>

<p>Selective inhibitor of the Src kinase family with subnanomolar IC50 values and good selectivity over c-Abl, PDGFRα and c-Kit kinases. The compound is effective in inhibiting growth in drug resistant cancer cell lines. In a recent study, it inhibited the growth of HER2-positive breast cancer cell lines which were resistant to pan-HER family kinase inhibitors such as lapatinib.</p>

<p>RET receptor tyroine kinase inhibitor</p>

<p>β3-adrenoceptor agonist</p>

<p>A Bad-like BH3 mimetic with strong affinity for Bcl-xl, Bcl-2 and Bcl-w that promotes BIM-mediated apoptosis. Enhanced efficacy when combined with other chemotherapies in xenograft models of B-cell malignancies and SCLC. Has senolytic effects on senescent cells, demonstrating revival of aged HSCs in vivo.</p>